O. Chambinremoussenard et al., SURFACE RECOVERY AND STRIPPING METHODS TO QUANTIFY PERCUTANEOUS-ABSORPTION OF CAFFEINE IN HUMANS, Journal of pharmaceutical sciences, 82(11), 1993, pp. 1099-1101
The percutaneous absorption of caffeine from two vehicles, an emulsion
and an acetone solution, was quantified by in vivo techniques in huma
ns. A surface recovery technique over a 6-h application and a strippin
g method after a 30-min application were performed on the volar aspect
of the forearm on 12 volunteers. Caffeine was assessed by HPLC. Two p
hases were distinguished in the percutaneous absorption of caffeine: a
higher filling up of the stratum corneum with the oil-in-water emulsi
on than with the acetone solution, which was then followed by a steady
-state flux corresponding to the penetration in the living tissues. Th
e permeability constants (K(p)) with emulsion and acetone were 1.59 .
10(-4) and 9.53 . 10(-8) cm/h, respectively. The stripping method show
ed concentrations of caffeine in stratum corneum that were five times
higher with emulsion (212 ng/cm2) than with acetone (37 ng/cm2). With
acetone as a vehicle, approximately 40% of caffeine of the cornified l
ayer was found around the treated area. This sizeable lateral spread w
ithin the stratum corneum was not observed with the emulsion.